528106
PI 3-Kγ Inhibitor
5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione
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EMD Chemicals, Inc.
480 S. Democrat Road
08027 Gibbstown
United States
Phone: 800 854 3417
Fax: 800 776 0999
E-mail: Customer.CareDesk@emdchemicals.com
09 February 2012
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A cell-permeable thiazolidinedione compound that acts as a potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase γ (PI 3-Kγ) (Ki = 7.8 nM; IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µM. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1 (IC50 = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.
| Product information | |||
|---|---|---|---|
| Form | Pink solid | ||
| Primary Target | PI 3-Kg | ||
| Primary Target Ki | 7.8 nM | ||
| Secondary target | IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively | ||
| Molar mass | 257.3 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Cell permeable | Yes | ||
| ATP Competitive | Yes | ||
| Purity | ≥90% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C12H7N3O2S | ||
| CAS number | 648450-29-7 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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